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Interstitial Cystitis (IC) is a chronic inflammatory disease that lacks effective treatment. The present study aimed to investigate the potential of aqueous ethanol extract of Cuminum cyminum (AEECC) on oxidative stress, inflammation and overactivity of urinary bladder induced by cyclophosphamide (CYP). Female Sprague-Dawley rats received intraperitoneal administration of cyclophosphamide (150â mg/kg, i. p. 1st , 4th , and 7th days). To investigate the urothelial damage, the bladder weight, nociception behavior, and Evans blue dye extravasation method was used. The antioxidants CAT, GPX and NO were measured. ELISA determined the IL-6 and TNF-α levels. The spasmolytic effect of AEECC was investigated on isolated bladder strips and its mechanisms were determined. The enhanced nociception behavior, bladder weight, vascular permeability, edema, hemorrhage, nitric oxide, IL-6 and TNF-α levels by CYP administration were significantly reduced by AEECC (250 and 500â mg/kg). A significant increase in serum antioxidant system such as CAT and GPx was also observed in AEECC-treated rats. The AEECC (3â mg/ml) significantly reduced urinary bladder tone in the strips pre-contracted with carbachol in both control and CYP-treated rats. This relaxation was demolished by atropine, nifedipine, glibenclamide, and indomethacin but not with propranolol. The plant extract showed the presence of antioxidant and anti-inflammatory phytochemicals. These results suggest that Cuminum cyminum offers uroprotective activity and can ameliorate CYP-induced bladder toxicity by modulating antioxidant parameters, pro-inflammatory cytokine levels and bladder smooth muscle overactivity. The in silico binding interactions of antioxidant 2I3Y and anti-inflammatory protein 1TNF with various ligands from Cuminum cyminum seeds revealed potential bioactive compounds with promising antioxidant and anti-inflammatory properties, providing valuable insights for drug development and nutraceutical research.
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Cuminum , Cistite , Ratos , Animais , Bexiga Urinária , Antioxidantes/farmacologia , Antioxidantes/uso terapêutico , Cistite/induzido quimicamente , Cistite/tratamento farmacológico , Citocinas , Fator de Necrose Tumoral alfa , Interleucina-6 , Ratos Sprague-Dawley , Ciclofosfamida/toxicidade , Anti-Inflamatórios/farmacologiaRESUMO
Global water consumption has grown twice as fast as the population. Wastewater is therefore a valuable and renewable source and provides additional water for priority uses. Wastewater can also be a source of pollution; thus, its physico-chemical and biological compositions can present major risks to the environment and human health. The objective of this study was to assess the status of irrigation waters in terms of salinization, accumulation of metallic elements, and microbiological contamination by parasites and pathogenic bacteria. The study focused on the surface water of Oued Fès used for irrigation located downstream of the industrial zone of Doukkarat and upstream of the industrial zone of Ain Noukbi (wastewater) before the confluence with the Oued Sebou, as well as on the treated wastewater of the wastewater treatment plant. The physico-chemical and microbiological analyses were carried out in two periods: summer and winter. Metals were analyzed by ICP-AES. The chemical and bacteriological quality of the wastewater and treated wastewater was found to be poor. These were characterized by organic pollution, including biodegradable pollutants, while upstream the organic residues were not biodegradables. COD, BOD5, Kjeldahl nitrogen, as well as chloride ion (Cl-) are above the standard values. The highest concentrations of Cd, at 850 µg/l, Cu, at 690 µg/l and Mn, at 470 µg/l, largely exceed the international standards and requirements. In addition to fecal contamination, characterized by total coliforms and thermo-tolerant coliforms, other pathogens were present, including helminth eggs, both in the wastewater and in the treated wastewater. Other pathogens, such as Vibrio cholera, were found at all three sites whether in winter or summer, with the exception of the downstream of Oued Fez in winter. As for Salmonella, it was present in treated wastewater during the winter only. The water used for irrigation upstream of Oued Fez and the treated wastewater have poor to very poor quality. Therefore, for a better use of these waters, it is necessary to ensure their regular treatment in order to minimize the impacts on the environment and human health.
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Águas Residuárias , Poluentes Químicos da Água , Humanos , Marrocos , Poluição Ambiental/análise , Metais/toxicidade , Metais/análise , Poluentes Químicos da Água/toxicidade , Poluentes Químicos da Água/análise , Água/análise , Monitoramento Ambiental , Irrigação AgrícolaRESUMO
This review summarizes available data on argan fruit botany, geographical distribution, traditional uses, environmental interest, socioeconomic role, phytochemistry, as well as health beneficial effects and examination of future prospects. In particular, ethnomedical uses of argan fruits are carried out throughout Morocco where it has been used against various diseases. Different classes of bioactive compounds have been characterized including essential oils, fatty acids, triacylglycerols, flavonoids and their newly reported acylglycosyl derivatives, monophenols, phenolic acids, cinnamic acids, saponins, triterpenes, phytosterols, ubiquinone, melatonin, new aminophenols along with vitamin E among other secondary metabolites. The latter have already shown a wide spectrum of in vitro, and ex vivo biologicalactivities including antioxidant, anti-inflammatory, anti-diabetic, antihypertensive, anti-hypercholesterolemia, analgesic, antimicrobial, molluscicidal anti-nociceptive and anticancer potential. Argan flesh (pulp) contains a broad spectrum of polyphenolic compounds which may have utility for incorporation into nutraceuticals and cosmeceuticals relevant to the food, cosmetic and health industries. Further research is recommended, especially on the health beneficial effects of the aminophenols.
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Frutas/química , Compostos Fitoquímicos/química , Compostos Fitoquímicos/farmacologia , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Sapotaceae/química , Frutas/metabolismo , Humanos , Metaboloma , Metabolômica/métodos , Marrocos , Fenóis/química , Óleos de Plantas/química , Sapotaceae/metabolismoRESUMO
A new phenolic-type compound containing a nitrogenous, heterocyclic-fused ring from the fruit of the argan tree, Argania spinosa (Skeels L.), is described. This and another already known compound also isolated in the course of the work belong to an obscure and rare class of natural products, the amino phenolics.
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Fenóis/química , Extratos Vegetais/química , Sapotaceae/química , Frutas/química , Espectroscopia de Ressonância Magnética , Espectrometria de Massas , Estrutura Molecular , Óleos de Plantas/química , ÁrvoresRESUMO
The purpose of this study was to evaluate the vitamin D status and determine the factors influencing it in the Drâa-Tafilalet community (southeastern Morocco). Sociodemographic factors, health, cognitive status, sun exposure, and nutritional conditions were examined to help us understand their association with vitamin D status. Vitamin D data were gathered through laboratory testing, while demographic and health information was collected through interviews with participants in 2023. The study involved 100 participants aged 60 and above, most of whom were women (85%) rather than men (15%). The majority of participants were Arabs (90%), with a minority being Amazigh (10%). The average vitamin D level was 31.83 ± 10.55 ng/mL, varying based on participants' age, education, and gender. Sun-exposed individuals exhibited significantly higher mean vitamin D levels (33.56 ± 11.99 ng/mL) compared to those with limited sun exposure (28.97 ± 9.28 ng/mL). Moreover, the time spent outdoors, seasonal changes, and the duration of sun exposure affected the levels of vitamin D. These findings depict the vitamin D status of the elderly population of Drâa-Tafilalet, recognized as one of Morocco's poorest regions, shedding light on the significant influencers. Nonetheless, additional research is necessary to explore the correlation between dietary habits, sunlight exposure, and vitamin D levels in both young and elderly populations.
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Estado Nutricional , Deficiência de Vitamina D , Vitamina D , Humanos , Marrocos , Masculino , Feminino , Pessoa de Meia-Idade , Vitamina D/sangue , Idoso , Deficiência de Vitamina D/epidemiologia , Deficiência de Vitamina D/sangue , Luz Solar , Fatores Sociodemográficos , Fatores Socioeconômicos , Nível de Saúde , Idoso de 80 Anos ou maisRESUMO
Colostrum is a nutritious milk synthesized by mammals during the postpartum period, and its rich bioactive components has led to a global increase in the consumption of bovine colostrum as a supplement. Bovine colostrum contains key components such as immunoglobulins, oligosaccharides, lactoferrin and lysozyme. It is a special supplement source due to its natural, high bioavailability and high concentrations of growth factors. Growth factors are critical to many physiological functions, and considering its presence in the colostrum, further research must be conducted on its safe application in many bodily disorders. Growth factors contribute to wound healing, muscle and bone development, and supporting growth in children. Additionally, the molecular mechanisms have been explored, highlighting the growth factors roles in cell proliferation, tissue regeneration, and the regulation of immune responses. These findings are crucial for understanding the potential health effects of bovine colostrum, ensuring its safe use, and forming a basis for future clinical applications. This review article examines the growth factors concentration in bovine colostrum, their benefits, clinical studies, and molecular mechanisms.
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Colostro , Peptídeos e Proteínas de Sinalização Intercelular , Colostro/química , Animais , Bovinos , Humanos , Peptídeos e Proteínas de Sinalização Intercelular/metabolismo , Feminino , Suplementos Nutricionais , GravidezRESUMO
Origanum grosii (L.) and Thymus pallidus (L.) are medicinal plants recognized for their uses in traditional medicine. In this context, the aim of this article is to highlight the results of a phytochemical analysis (HPLC), with particular emphasis on the antioxidant (DPPH, TAC, and FRAP), analgesic, anti-inflammatory, haemagglutinin-test-related, and hemolytic activities of the total extracts of these plants. Phytochemical analysis via HPLC revealed that licoflavone C (30%) is the main compound in Origanum grosii, while hesperidin (43%) is found in T. pallidus. Evaluation of the antioxidant capacity of Origanum grosii and Thymus pallidus using the DPPH, TAC, and FRAP methods revealed an IC50 of the order of 0.085 mg/mL and 0.146 mg/mL, an EC50 of the order of 0.167 mg/mL and 0.185 mg/mL, and a total antioxidant capacity of between 750 mg EQ/g and 900 mg EQ/g, respectively. Analgesic evaluations revealed writhes inhibition of the order of 97.83% for O. grosii and 90% for T. pallidus. In addition, both plant extracts showed limited hemolytic activity, not exceeding 30% at a concentration of 100 mg/mL. Evaluation of the anti-inflammatory potential showed edema inhibition of the order of 94% (800 mg/kg) for O. grosii and 86% (800 mg/kg) for T. pallidus. These results highlight the potential applications of these extracts in pharmacological research.
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AIMS: The present study aimed to provide summarized data related to the phytocompouds improving glucose uptake in the diabetic state. BACKGROUND: Glucose uptake in peripheral tissues such as skeletal muscle and adipose tissue is considered as an important step in the regulation of glucose homeostasis. Reducing high blood glucose levels in diabetic patients via targeting peripheral glucose uptake is a promising strategy to develop new antidiabetic medications derived from natural products. OBJECTIVE: The current review focused on antidiabetic natural phytocompounds acting on glucose uptake in adipocytes and skeletal muscles to highlight their phytochemistry, the mechanistic pathway involved, toxicity, and clinical assessment. METHODS: A systematic search was conducted in the scientific database with specific keywords on natural phytocompounds demonstrated to possess glucose uptake stimulating activity in vitro or ex vivo during the last decade. RESULTS: In total, 195 pure molecules and 7 mixtures of inseparable molecules isolated from the plants kingdom, in addition to 16 biomolecules derived from non-herbal sources, possess a potent glucose uptake stimulating capacity in adipocytes and/or skeletal muscles in adipocytes and/or skeletal muscles in vitro or ex vivo. Molecular studies revealed that these plant-derived molecules induced glucose uptake via increasing GLUT-4 expression and/or translocation through insulin signaling pathway, AMPK pathway, PTP1B activity inhibition or acting as partial PPARγ agonists. These phytocompounds were isolated from 91 plants, belonging to 57 families and triterpenoids are the most sous-class of secondary metabolites showing this activity. Among all the phytocompounds listed in the current review, only 14 biomolecules have shown an interesting activity against diabetes and its complications in clinical studies. CONCLUSION: Epicatechin, catechin, epigallocatechin 3-gallate, quercetin, quercetin 3-glucoside, berberine, rutin, linoleic acid, oleanolic acid, oleic acid, chlorogenic acid, gallic acid, hesperidin, and corosolic acid are promising phytocompounds that showed great activity against diabetes and diabetes complications in vitro and in vivo. However, for the others phytocompounds further experimental studies followed by clinical trials are needed. Finally, foods rich in these compounds cited in this review present a healthy diet for diabetic patients.
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Glucose , Hipoglicemiantes , Humanos , Glucose/metabolismo , Hipoglicemiantes/farmacologia , Hipoglicemiantes/uso terapêutico , Hipoglicemiantes/química , Insulina/metabolismo , Quercetina/farmacologia , Transdução de Sinais , Transporte Biológico/efeitos dos fármacosRESUMO
The disease-free existence of humans is constantly under attack by a variety of infections caused by a variety of organisms including bacteria. Notable among the bacteria is Staphylococcus aureus which is an etiological organism for infections including impetigo, folliculitis, and furuncles. The response of the human immune system against this disease is often neutralized by the production of a pigment called Staphyloxanthin (STX) via a series of reactions mediated by several enzymes. Among these enzymes, dehydrosqualene synthase, also known as CrtM, has emerged as a viable drug target due to its role in mediating the first step of the pathway. Consequently, this study employs molecular modeling approaches including molecular docking, quantum mechanical calculations, and molecular dynamics (MD) simulations among others to investigate the potential of napthyridine derivatives to serve as inhibitors of the CrtM. The results of the study revealed the high binding affinities of the compounds for the target as demonstrated by their docking scores, while further subjection to screening pipeline aimed at determining their fitness for development into drugs revealed just one compound namely 6-[[1-[(2-fluorophenyl) methyl]triazol-4-yl]methoxy]-4-oxo-1H-1,5-naphthyridine-3-carboxylic acid as the compound with good drug-like, pharmacokinetics, and toxicity properties profiles. A 100 ns-long MD simulation of the complexes formed after molecular docking revealed the stable interaction of the compound with the target. Ultimately, this study can be a promising outlet to discover a weapon to fight against clinically resistant bacteria, however, further experimental studies are suggested to carry out in the wet lab, pre-clinical, and clinical levels.
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Thymus atlanticus (Lamiaceae) is a plant endemic to the Mediterranean basin that is found in significant quantities in the arid regions of Morocco. Thymus atlanticus is used in traditional medicine to treat infectious and non-infectious diseases. It is also used for the isolation of essential oils and for the seasoning of many dishes in the Mediterranean diet. The major constituents of Thymus atlanticus are saponins, flavonoids, tannins, alkaloids, various simple and hydroxycinnamic phenolic compounds, and terpene compounds. Several of these compounds act on signaling pathways of oxidative stress, inflammation, and blood sugar, which are parameters often dysregulated during aging. Due to its physiochemical characteristics and biological activities, Thymus atlanticus could be used for the prevention and/or treatment of age-related diseases. These different aspects are treated in the present review, and we focused on phytochemistry and major age-related diseases: dyslipidemia, cardiovascular diseases, and type 2 diabetes.
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In an attempt to examine novel adsorbents in accessing an ideal adsorption system, this study aimed to help understand the main and secondary characteristics of a Moroccan natural clay. X-ray fluorescence, infrared, and scanning electron microscopy with energy-dispersive X-ray spectroscopy analysis (SEM-EDX) were used for the identification. The findings demonstrate that this Clay is composed of a mixture of quartz, calcite, magnetite, and Rutile in very high proportions. SEM revealed the presence of clay grains in the presence of fine particles and irregularly contoured sticks. The results of semiquantitative detection by EDX also reveal the presence of certain mineral species (Si, Al, Mg, Fe, K, Cl, S, Ca, and Na). The exploited kinetic technique was achieved using two different kinetic models: first- and second-order rate laws. Commensurate to the obtained results, the 2-sec order model better described the adsorption of dye MB onto the natural clay. The results confirmed that the adsorption process followed the Langmuir model with the high coefficient correlation obtained which are very close to 1. In the sequel, DFT results revealed that the HOMO and LUMO surfaces of the methylene blue dye are mostly distributed on all dye parts, reflecting possible strong interactions with the clay. The quantum descriptors investigated in this study identify the most nucleophilic and electrophilic centers that can be used to suggest a suitable mechanism for the adsorption of the dye by the clay. The values of enthalpy ΔH0 and entropy ΔS0 of activation were -15.88 kJ mol-1 and -0.021 J mol-1 K-1, respectively, show that the nature of the adsorption process of MB on clay is exothermic and the order of distribution of the dye molecules on the adsorbent increases with respect to that of the solution so the negative values of ΔG0 (from -9. 62 to -8.99 kJ mol-1) indicate that the adsorption process is spontaneous.
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Breast cancer (BC) is the most common female cancer in terms of incidence and mortality worldwide. Tamoxifen (Nolvadex) is a widely prescribed, oral anti-estrogen drug for the hormonal treatment of estrogen-receptor-positive BC, which represents 70% of all BC subtypes. This review assesses the current knowledge on the molecular pharmacology of tamoxifen in terms of its anticancer and chemo-preventive actions. Due to the importance of vitamin E compounds, which are widely taken as a supplementary dietary component, the review focuses only on the potential importance of vitamin E in BC chemo-prevention. The chemo-preventive and onco-protective effects of tamoxifen combined with the potential effects of vitamin E can alter the anticancer actions of tamoxifen. Therefore, methods involving an individually designed, nutritional intervention for patients with BC warrant further consideration. These data are of great importance for tamoxifen chemo-prevention strategies in future epidemiological studies.
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This study aims to investigate the chemical and mineral composition, antioxidant, analgesic, and anti-inflammatory effects of the aqueous extract of Cistus laurifolius var. atlanticus Pit. (Cistaceae). Additionally, molecular docking interactions of various ligands with antioxidant protein target urate oxidase (1R4U) and anti-inflammatory protein target cyclooxygenase-2 (3LN1), revealing potential dual activities and highlighting specific residue interactions. The chemical characterization focused at first glance on the mineral composition which showed that C. laurifolius extract is a mineral-rich source of potassium (K), magnesium (Mg), manganese (Mn), sodium (Na), phosphorus (P), and zinc (Zn). We next performed, ultra-performance liquid chromatography-tandem mass spectrometry (UPLC-MS/MS) analysis, the latter showed various polyphenols in C. laurifolius extract including Gallic acid as the predominant polyphenol. Isoquercetin, Taxifolin and Astragalin were also among the major flavonoids detected. The antioxidant capacity of C. laurifolius leaves was tested using 2,2'-azino-bis (3-ethylbenzothiazoline-6-sulfonic acid) (ABTS), 2,2-diphenyl-1- picrylhydrazyl (DPPH) and reducing power (RP) assays. In vitro analysis of the anti-inflammatory property of C. laurifolius leaves was conducted by the albumin denaturation test and the in vivo was assessed in the sequel by carrageenan-induced paw edema test. The analgesic activity was evaluated in vivo using tail flick, acetic acid-induced contortion, and plantar tests. The findings showed that the leave extract had a powerful antioxidant activity with an IC50 values of 2.92 ± 0.03 µg/mL (DPPH) and 2.59 ± 0.09 µg/mL (in RP test). The studied extract strongly abolished the induced inflammation (82%). Albumin denaturation test recorded an IC50 value of 210 µg/mL. Importantly, the oral administration of C. laurifolius extract considerably reduced the nociceptive effect of acetic acid in rats, showing a significant analgesic effect in a dose-related manner. Altogether, our results showed that C. laurifolius can be a promising source of phytochemicals for drug development potential.
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Antioxidantes , Cistus , Ratos , Animais , Antioxidantes/farmacologia , Antioxidantes/análise , Cistus/química , Polifenóis/farmacologia , Polifenóis/análise , Cromatografia Líquida , Simulação de Acoplamento Molecular , Extratos Vegetais/farmacologia , Extratos Vegetais/química , Espectrometria de Massas em Tandem , Analgésicos/farmacologia , Analgésicos/química , Anti-Inflamatórios/farmacologia , Anti-Inflamatórios/química , Ácido Acético , Minerais , AlbuminasRESUMO
Coumadin (R-, S-warfarin) is a challenging drug to accurately dose, both initially and for maintenance, because of its narrow therapeutic range and wide interpatient variability and is typically administered as a racemic (Rac) mixture, which complicates the biotransformation pathways. The goal of the current work was to identify the human UDP-glucuronosyltransferases (UGTs) involved in the glucuronidation of the separated R- and S-enantiomers of 6-, 7-, and 8-hydroxywarfarin and the possible interactions between these enantiomers. The kinetic and inhibition constants for human recombinant 1A family UGTs toward these separated enantiomers have been assessed using high-performance liquid chromatography (HPLC)-UV-visible analysis, and product confirmations have been made using HPLC-mass spectrometry/mass spectrometry. We found that separated R- and S-enantiomers of 6-, 7-, and 8-hydroxywarfarin demonstrate significantly different glucuronidation kinetics and can be mutually inhibitory. In some cases significant substrate inhibition was observed, as shown by K(m), V(max), and K(i), comparisons. In particular, UGT1A1 and extrahepatic UGT1A10 have significantly higher capacities than other isoforms for S-7-hydroxywarfarin and R-7-hydroxywarfarin glucuronidation, respectively. Activity data generated using a set of well characterized human liver microsomes supported the recombinant enzyme data, suggesting an important (although not exclusive) role for UGT1A1 in glucuronidation of the main warfarin metabolites, including Rac-6- and 7-hydroxywarfarin and their R- and S-enantiomers in the liver. This is the first demonstration that the R- and S-enantiomers of hydroxywarfarins are glucuronidated, with significantly different enzymatic affinity and capacity, and supports the importance of UGT1A1 as the major hepatic isoform involved.
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Glucuronídeos/metabolismo , Glucuronosiltransferase/metabolismo , Microssomos Hepáticos/enzimologia , Varfarina/análogos & derivados , Cromatografia Líquida de Alta Pressão , Humanos , Cinética , Microssomos Hepáticos/metabolismo , Proteínas Recombinantes/metabolismo , Espectrofotometria Ultravioleta , Estereoisomerismo , Espectrometria de Massas em Tandem , Bancos de Tecidos , Varfarina/isolamento & purificação , Varfarina/metabolismoRESUMO
This work aimed to characterize and compare the physicochemical, ascorbic acid, phenolic, and flavonoid compounds, as well as the antioxidant properties, pollen spectra, and sugar profiles of twenty-three organic honeys produced in the Middle Atlas of Morocco. As results, the pollen analysis showed 22 taxa and revealed the dominance of Ziziphus lotus pollens for all monofloral honeys. The moisture content ranged from 15.9 to 19.0%, pH values werebetween 3.9 and 4.8, electrical conductivity varied from 100 to 581 µs/cm, ash content varied from 0.1 to 2.4%, and the invertase activity ranged from 3.5 to 36 U/kg. Moreover, hydroxymethylfurfural(HMF) varied from 1.2 to 13.5 mg/kg, which confirmed the freshness of our honey samples. For the sugar profiles, there were no significant differences between the examined groups of honeys (p > 0.05) for both fructose and glucose. Additionally, our study showed good antioxidant properties (total antioxidant activity ranged from 34.18 to 131.20 mg AAE/g; DPPH IC50 values ranged from 8.14 to 45.20 mg/mL; ABTS IC50 values ranged from 8.19 to 32.76 mg/mL) and high amounts of phenolic compounds ranging between 20.92 ± 0.03 and 155.89 ± 0.03 mg GAE/100 g, respectively; flavonoid compounds ranged from 5.52 to 20.69 mg QE/100 g, and ascorbic acid ranged from 8.01 to 23.26 mg/100 g. Overall, the proximate composition and the general characterization of organic monofloral and polyfloral honeys as sustainable and health-promising functional products may increase their commercial values, promote their marketability, and might have a significant impact on the basic circular/sustainable economy as a solid lever for solidarity economic development, especially in the rural/poor Moroccan communities. The investigated features may allow and support the incorporation of Moroccan organic honeys and their biovaluable ingredients in the nutraceutical and food industries for multiple purposes.
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Background: Multidrug resistance (MDR) and extensively drug-resistant (XDR) are now the biggest threats to human beings. Alternative antimicrobial regimens to conventional antibiotic paradigms are extensively searched. Although Cistus extracts have long been used for infections in traditional folk medicines around the world, their efficacy against resistant bacteria still needs to be elucidated. We aim to investigate the antibiotic susceptibility profiles of clinical strains Enterococcus faecium, Staphylococcus aureus, Klebsiella pneumoniae, Acinetobacter baumannii, Pseudomonas aeruginosa, and Enterobacter cloacae (acronym "ESKAPE"), and their resistance mechanisms by PCR, as well as their sensitivity to C. monspeliensis (CM) and C. salviifolius (CS) methanol extracts and their fractions. Methods: Antibiotic susceptibility profile and resistance mechanism were done by antibiogram and PCR. Fractions of CM and CS were obtained using maceration and Soxhlet; their antibacterial activities were evaluated by determining inhibition zone diameter (IZD), minimum inhibitory concentration (MIC), and minimum bactericidal concentration (MBC). Results: Results revealed that all strains were XDR except S. aureus, which was MDR. The PCR indicates the presence of gene-mediated resistance (bla CTX-M, bla SHV, bla OXA-48, bla NDM, bla OXA-51, bla OXA-58, bla IMP, bla VIM, and bla mecA). Also, maceration was slightly better for bioactivity preservation. Overall, the extracts of CM (IZD = 20 mm, MIC = 0.01 mg/mL) were more active than those of CS. All extracts inhibited MRSA (methicillin-resistant Staphylococcus aureus) and ERV (Enterococcus faecium Vancomycin-Resistant) with interesting MICs. The ethyl acetate fraction manifested great efficacy against all strains. Monoterpene hydrocarbons and sesquiterpenes oxygenated were the chemical classes of compounds dominating the analyzed fractions. Viridiflorol was the major compound in ethyl acetate fractions of 59.84% and 70.77% for CM and CS, respectively. Conclusions: The superior activity of extracts to conventional antibiotics was seen for the first time in the pathogens group, and their bactericidal effect could be a promising alternative for developing clinical antibacterial agents against MDR and XDR ESKAPE bacteria.
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Centaurea calcitrapa has been intensively utilized in ethnomedicinal practices as a natural therapeutic recipe to cure various ailments. The current study aimed to chemically characterize ethanolic extract of C. calcitrapa (EECC) aerial parts (leaves and shoots) by use of gas chromatography-mass spectrometry analyses (GC-MS) and investigate its antioxidant and in vitro anticancer activities, elucidating the underlying molecular mechanism by use of flow cytometry-based fluorescence-activated cell sorting (FACS) and conducting in silico assessment of binding inhibitory activities of EECC major compounds docked to caspase-3. CG-MS profiling of EECC identified a total of 26 major flavonoids and polyphenolic compounds. DPPH and ABTS assays revealed that EECC exhibits potent antioxidant activity comparable to standard reducing agents. Results of the proliferation assay revealed that EECC exhibit potent, dose-dependent cytotoxic activities against triple-positive (MCF-7) and triple-negative (MDA-MB-231) breast cancer cell models, with IC50 values of 1.3 × 102 and 8.7 × 101 µg/mL, respectively. The observed cytotoxic effect was specific to studied cancer cells since EECC exhibited minimal (~<10%) cytotoxicity against MCF-12, a normal breast cell line. FACS analysis employing annexin V-FITC/propidium iodide double labeling demonstrated that the observed anti-proliferative activity against MCF-7 and MDA-MB-231 was mediated via apoptotic as well as necrotic signaling transduction processes. The increase in fluorescence intensity associated with DCFH oxidation to DCF, as reported by FACS, indicated that apoptosis is caused by generation of ROS. The use of caspase-3-specific fluorogenic substrate revealed a dose-dependent elevation in caspase-3 substrate-cleavage activity, which further supports EECC-mediated apoptosis in MCF-7 cells. The major EECC compounds were examined for their inhibitory activity against caspase-3 receptor (1HD2) using molecular docking. Three compounds exhibited the highest glide score energy of −5.156, −4.691 and −4.551 kcal/mol, respectively. Phenol, 2,6-dimethoxy established strong binding in caspase-3 receptor of hydrogenic type, with residue ARG 207 and of PI-PI stacking type with residue HIS 121. By contract, hexadecenoic acid showed 3 H-bond with the following residues: ASN 615, ASN 616a and THR 646. Taken together, the current findings reveal that EECC exhibits significant and specific cytotoxicity against breast cancer cells mediated by the generation of ROS and culminating into necrosis and apoptosis. Further investigations of the phytoconstituents-rich C. calcitrapa are therefore warranted against breast as well as other human cancer cell models.
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Saffron (Crocus sativus L.) is a medicinal plant, originally cultivated in the East and Middle East, and later in some Mediterranean countries. Saffron is obtained from the stigmas of the plant. Currently, the use of saffron is undergoing a revival. The medicinal virtues of saffron, its culinary use and its high added value have led to the clarification of its phytochemical profile and its biological and therapeutic characteristics. Saffron is rich in carotenoids and terpenes. The major products of saffron are crocins and crocetin (carotenoids) deriving from zeaxanthin, pirocrocin and safranal, which give it its taste and aroma, respectively. Saffron and its major compounds have powerful antioxidant and anti-inflammatory properties in vitro and in vivo. Anti-tumor properties have also been described. The goal of this review is to present the beneficial effects of saffron and its main constituent molecules on neuropsychiatric diseases (depression, anxiety and schizophrenia) as well as on the most frequent age-related diseases (cardiovascular, ocular and neurodegenerative diseases, as well as sarcopenia). Overall, the phytochemical profile of saffron confers many beneficial virtues on human health and, in particular, on the prevention of age-related diseases, which is a major asset reinforcing the interest for this medicinal plant.
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Crocus , Plantas Medicinais , Envelhecimento , Crocus/química , Humanos , Nutrientes , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Extratos Vegetais/uso terapêuticoRESUMO
AIM: This study aimed to investigate the effect of Micromeria graeca on blood glucose levels and lipid parameters in an experimental model of diabetes. BACKGROUND: Micromeria graeca (L.) Benth. ex Rchb is a medicinal plant used in Morocco for the treatment of several pathologies including diabetes. OBJECTIVE: This study aimed to evaluate the antihyperglycemic and antihyperlipidemic effects of the aqueous extract of Micromeria graeca (M. graeca) aerial parts (AEMG) under physiological (normal rats) and pathological (STZ-induced diabetic rats) conditions. Additionally, we analyzed the phytochemical composition and antioxidant capacity. METHODS: The effects of the acute and sub-chronic administration of AEMG (20 mg/kg) on blood glucose levels and lipid profiles were evaluated in normal and streptozotocin-induced diabetic rats. Moreover, the phytochemical analysis was carried with standard tests and estimation of total phenolics compounds by Folin-Ciocalteu reagent. The antioxidant activity was realized by the DPPH method. RESULTS: Single oral administration of M. graeca aqueous extract decreased blood glucose levels 4 and 6 hours (p<0.01) after treatment in diabetic rats. In accordance, the repeated oral administration of M. graeca showed a significant reduction in blood glucose levels in diabetic rats since the second day to the end of the period experiment (p<0.0001). In addition, two weeks of treatment with M. graeca reduced total cholesterol levels (p<0.05) with a significant increase of HDL-c level (p<0.01) in diabetic rats. Moreover, M. graeca scavenged DPPH radical in a dose-dependent manner (IC50=0.48 mg/ml), whereas IC50 was 0.55 mg/ml for BHT. Phytochemical analysis showed the richness of Micromeria graeca on polyphenols (281.94±4.61 mg GAE/1 g), flavonoids, tannins, glycosides, saponins, sterols, sesquiterpenes, and terpenoids. CONCLUSION: AEMG exhibits antihyperglycemic and antihyperlipidemic activities in STZ-induced diabetic rats and a potent antioxidant capacity.